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apalutamide + goserelin
- Development stage
- Unknown
- Lead developer
- Janssen Pharmaceutical
- Modality
- Peptides, Small Molecules
- Administration
- Oral, Subcutaneous
01
Overview
A combination therapy consisting of the androgen receptor antagonist apalutamide and the gonadotropin-releasing hormone (GnRH) agonist goserelin. This regimen is being investigated for the treatment of androgen receptor (AR)-expressing locally advanced or recurrent/metastatic salivary gland carcinoma (SGC). Apalutamide is a nonsteroidal antiandrogen that acts as a selective competitive antagonist of the androgen receptor, blocking androgen-mediated gene transcription and nuclear translocation. Goserelin is a synthetic decapeptide analogue of GnRH that, upon chronic administration, leads to down-regulation of the pituitary GnRH receptors, resulting in a decrease in luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion, and a subsequent fall in serum testosterone levels to castrate levels. The combination aims to achieve maximal androgen blockade in AR-positive SGC, a rare malignancy that shares biological similarities with prostate cancer.
- Brand names
- ErleadaZoladex
- Other names
- Apalutamide plus GnRH AgonistYATAGARASU regimen
02
Targets
GnRHR (Gonadotropin-releasing hormone receptor)GABRR (GABA-A receptor subunit rho)AR (Adrenergic receptors)
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